“If this blog helped you out, don’t keep it to yourself—share the link on your socials!” 👍 “Like what you read? Spread the love and share this blog on your social media.” 👍 “Found this useful? Hit share and let your friends know too!” 👍 “If you enjoyed this post, please share the URL with your friends online.” 👍 “Sharing is caring—drop this link on your social media if it helped you.”

Sunday, July 27, 2025

Calcipotriol


Calcipotriol (also known as calcipotriene in the US) is a topical synthetic vitamin D3 analogue used primarily for the treatment of plaque psoriasis. It exerts its therapeutic effect by regulating keratinocyte proliferation and differentiation, leading to reduced epidermal hyperplasia and inflammation. Calcipotriol is not used systemically due to its potential to disturb calcium metabolism when absorbed in large amounts, but it is generally safe when applied in regulated topical quantities.

This profile provides a professional and detailed overview of calcipotriol, including its pharmacological properties, mechanism of action, clinical uses, administration, precautions, adverse effects, and drug interactions.

Pharmacological Classification

  • Therapeutic class: Anti-psoriatic agent

  • Pharmacologic class: Vitamin D analogue

  • ATC code: D05AX02

  • Legal status: Prescription-only medicine (Rx)

Brand Names and Formulations

  • Brand names: Dovonex®, Daivonex®, Sorilux®, Psorcutan®

  • Available forms:

    • Topical cream (50 micrograms/g)

    • Topical ointment

    • Scalp solution or foam

    • Fixed-dose combination with corticosteroids (e.g., calcipotriol + betamethasone dipropionate: Dovobet®, Enstilar®)

Mechanism of Action

Calcipotriol is a synthetic derivative of calcitriol (1,25-dihydroxyvitamin D3). It binds to vitamin D receptors (VDR) in keratinocytes, influencing gene transcription involved in cell proliferation and immune function. Its primary mechanisms include:

  • Inhibition of keratinocyte proliferation, which is exaggerated in psoriasis

  • Induction of keratinocyte differentiation, helping normalize epidermal cell turnover

  • Modulation of cytokine production, reducing skin inflammation

  • Inhibition of T-cell activity and pro-inflammatory cytokines (e.g., IL-2, IL-6)

These effects result in:

  • Thinner psoriatic plaques

  • Reduced erythema and scaling

  • Decreased epidermal hyperplasia

Calcipotriol has about 100–200 times less effect on calcium metabolism than natural vitamin D3, minimizing the risk of hypercalcemia with topical use.

Indications

Approved Uses

  • Plaque psoriasis (psoriasis vulgaris):

    • Mild-to-moderate cases: monotherapy

    • Moderate-to-severe cases: in combination with corticosteroids

Off-label / Investigational Uses

  • Scalp psoriasis

  • Palmoplantar psoriasis

  • Inverse psoriasis (intertriginous areas, often in reduced concentrations)

  • Psoriatic nail disease (topical penetration limited; may be combined with other therapies)

Dosage and Administration

Adults and Adolescents ≥12 years

  • Apply twice daily to affected areas (morning and evening)

  • Maximum weekly dose:

    • Cream or ointment: 100 g/week

    • Scalp solution: 60 mL/week

  • In fixed combination with betamethasone: typically applied once daily

  • Improvement is often seen within 2 weeks, with optimal results by 8 weeks

Children (under 12 years)

  • Not routinely recommended due to risk of calcium metabolism effects

  • If used, close monitoring is required

Application Instructions

  • Apply a thin layer to the affected skin

  • Avoid application on face, eyes, or genitals

  • Wash hands thoroughly after use

  • Do not use under occlusive dressings unless directed

  • Compatible with moisturizers but should be applied at separate times

Contraindications

  • Known hypersensitivity to calcipotriol or any excipients

  • Disturbances in calcium metabolism, e.g., hypercalcemia, hypervitaminosis D

  • Severe hepatic or renal impairment (systemic absorption risk)

  • Erythrodermic, exfoliative, or pustular psoriasis (not indicated)

Warnings and Precautions

  • Avoid excessive use: Risk of hypercalcemia if applied over large body surface areas or beyond maximum weekly dose

  • UV light exposure: Use with caution alongside phototherapy due to potential cumulative effect

  • Avoid facial use: High risk of irritation

  • Wash hands after application to prevent unintended spread to face or mucous membranes

  • Use with caution in pediatric patients and only under medical supervision

Adverse Effects

Common (≥1%)

  • Skin irritation (burning, itching, erythema at application site)

  • Peeling, dryness, or rash

  • Worsening of psoriasis in some cases

  • Contact dermatitis (less common than with corticosteroids)

Uncommon (<1%)

  • Hypercalcemia (reversible upon discontinuation)

  • Photosensitivity

  • Facial or perioral dermatitis (due to accidental application or transfer)

  • Changes in serum calcium or urinary calcium (usually with prolonged or excessive use)

Rare

  • Urticaria, angioedema

  • Allergic reactions

  • Hypercalciuria without overt hypercalcemia

Drug Interactions

  • Systemic calcium supplements or vitamin D analogs: May increase risk of hypercalcemia

  • Corticosteroids (topical): Often combined with calcipotriol for synergistic effect; monitor for local side effects

  • Phototherapy: Use cautiously to avoid enhanced photosensitivity

  • No known significant CYP-mediated systemic interactions as systemic absorption is minimal under normal use

Use in Pregnancy and Lactation

Pregnancy

  • Category C (Australia), not classified in the UK

  • Use only if clearly needed and if potential benefit outweighs risk

  • Animal studies suggest potential skeletal developmental toxicity at high doses

Breastfeeding

  • Unknown whether calcipotriol is excreted in human milk

  • If used, avoid application to the chest area to prevent infant exposure

  • Prefer short-term localized use during lactation

Use in Special Populations

  • Elderly: No specific adjustments needed

  • Pediatrics: Limited data for children under 12; caution due to systemic absorption risk

  • Renal/hepatic impairment: Avoid excessive use due to risk of impaired drug clearance and hypercalcemia

Fixed-Dose Combination Therapies

Calcipotriol is commonly used in fixed combination with betamethasone dipropionate, a potent corticosteroid, for enhanced efficacy and reduced irritation.

  • Advantages:

    • Better efficacy than either agent alone

    • Reduced risk of irritation compared to calcipotriol monotherapy

    • Once-daily application improves compliance

  • Examples:

    • Dovobet®, Enstilar® (foam), Taclonex®

Clinical Efficacy

  • Calcipotriol significantly improves PASI (Psoriasis Area and Severity Index) scores in mild to moderate psoriasis

  • Comparable efficacy to class II corticosteroids

  • Maintenance therapy may reduce relapse risk after corticosteroid tapering

  • In scalp psoriasis, foam formulations offer better penetration and cosmetic acceptability

Patient Counseling Points

  • Apply exactly as prescribed, no more than recommended

  • Do not use on face, genitals, or damaged skin

  • Report any signs of excessive irritation, redness, or burning

  • Use sunscreen and limit UV exposure (natural and artificial)

  • Do not cover treated areas with occlusive dressings

  • Inform doctor of calcium supplements or vitamin D use

  • Discontinue and report if signs of systemic effects (nausea, muscle weakness, confusion) arise

  • Store at room temperature and keep out of reach of children




on
Labels:

No comments:

Post a Comment

Subscribe to: Post Comments (Atom)